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238 results on '"Amico Roxas M"'

5. Synthesis and pharmacological properties of benzothiazole, 1,3-4-oxadiazole and 1,3,4-thiadiazole derivatives

Author

Santagati, M, Modica, Maria Nunziata, Santagati, A, Russo, F, Caruso, A, Cutuli, V, DI PIETRO, E, and AMICO ROXAS, M.

Subjects
Male, Oxadiazoles, Behavior, Animal, Anti-Inflammatory Agents, Non-Steroidal, Carrageenan, Rats, Lethal Dose 50, Rats, Sprague-Dawley, Mice, Thiazoles, Thiadiazoles, Animals, Edema, Benzothiazoles, Stomach Ulcer, Pain Measurement
Abstract

The reaction of the 2-amino-substituted 1,3,4-oxadiazoles 9, 10 and the benzothiazoles 11, 12 with ethyl cyanoacetate is described. The obtained cyanoacetamide derivatives 13-16 gave the benzylidene derivatives 18-21 by condensation with benzaldehyde. 2-Phenyl-5-amino-1,3,4-oxadiazolo[3,2-a]pyrimidin-7-one (17) was also obtained. Moreover, the preparation of 6,7,8,9-tetraydro-5H-1,3,4-thiadiazolo[2,3-b]quinazolin++ +-5-thio-derivatives 22-25 and N-(1,3,4-thiadiazol-2-yl-5-substituted)-3,4-5,6-tetrahydro-anthran ilic acids 26-29 is also described. All above compounds and compounds, related to them, 1-8 were tested for their analgesic and antiinflammatory activities and the pharmacological screening results are reported and discussed.

Published
1994

33. Protective effect of propionyl-l-carnitine against paf-induced rat paw oedema

Author

Caruso, A., Cutuli, V.M.C., de Bernardis, E., Leonardi, G., and Amico-Roxas, M.

Abstract

Recent reports from our laboratory gave evidence showing that propionyl-l-carnitine (PLC), unlike l-carnitine (LC) and acetyl-l-carnitine (ALC), has anti-inflammatory activity in some models of vascular inflammation in rodents. The present paper shows that PLC (50 to 200 mg kg−1 i.p.) inhibits rat paw oedema induced by platelet activating factor (PAF), while LC and ALC, as well as indomethacin and phenylbutazone, are ineffective. The extent of the maximal inhibition produced by PLC at 200 mg kg−1 was comparable to that of betamethasone 0.05 mg kg−1 or sodium salicylate 100 mg kg−1. PLC inhibited also the early phase (1–2 h) of carrageenin-induced rat paw oedema, which is partly dependent on PAF release, but it was ineffective in the eicosanoid-dependent late phase (3–4 h) of the carrageenin oedema. We suggest that such anti-inflammatory activity of PLC may be due to various mechanisms converging on a stabilizing action upon biomembranes.

Published
1995
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36. LPROPIONYL CARNITINE AN ENDOGENOUS ESTER IN FATTY ACID METABOLISM EXERTS ANTISHOCK AND ENDOTHELIAL PROTECTIVE EFFECTS IN RAT SPLANCHNIC ISCHEMIAREPERFUSION INJURY

Author

Stroh, Rebecca, Christopher, Theodore A., Lopez, Bernard L., Guo, Ya-Ping, Amico-Roxas, M., and Ma, Xin-Liang

Abstract

Splanchnic artery occlusion (SAO) results in a severe form of circulatory shock in which oxygen-derived free radicals play an important role. L-Propionyl carnitine (LPC), an endogenous ester that plays a crucial role in cellular fatty acid oxidation and metabolism, has been shown to exert a protective effect in myocardial ischemia/reperfusion injury. Our purpose was to investigate the effects of LPC in an SAO model of ischemia/reperfusion injury. Pentobarbital-anesthetized rats were subjected to 60 min of SAO followed by 120 min of reperfusion. An intravenous bolus of LPC (200 μg/kg) administered 2 min before reperfusion prolonged survival time (116 ± 4 vs. 81 ± 3 min in 1 mL/kg .9 NaCl vehicle, p< .01), increased survival rate (88 vs. 13.6, p< .01), and attenuated the percent increase in hematocrits (27 ± 4 vs. 43 ± 3, p< .05), and the increases in tissue myeloperoxidase activity (1.76 ± .4 U/100 mg vs. 3.79 ± .2 U/100 mg, p< .05). In addition, LPC increased mean arterial blood pressures at 60 min (p< .05), 80 min (p< .05), 100 min (p< .05), and 120 min (p< .05) postreperfusion. Moreover, LPC markedly attenuated splanchnic artery endothelial dysfunction induced by SAO ischemia/reperfusion injury (maximal vasorelaxation to ACh, 74 ± 2.7 vs. 57 ± 1.9 in vehicle, p< .01). In this murine SAO model of ischemia/reperfusion injury, LPC affords significant protection that may be achieved through inhibiting leukocyte infiltration into intestinal tissue and preserving endothelial function, thereby decreasing micro-vascular permeability and maintaining tissue perfusion.

Published
1998

40. [Reactivity of 3-aryl-4-amino-5-mercapto-4H-1,2,4-triazoles: synthesis and biological evaluation of 3,6-diaryl derivatives of 7H-1,2,4-thiazole[3,4-b][1,3,4]thiadiazines, of 3-aryl-4-amino-5-carboxymethylthio-4H-1,2,4-triazoles]

Author

Mazzone, G., Bonina, F., Panico, A. M., Amico-Roxas, M., Caruso, A., Giovanna BLANDINO, and Vanella, A.

Subjects
Male, Analgesics, Antifungal Agents, Chemical Phenomena, Thiadiazines, Anti-Inflammatory Agents, Non-Steroidal, Fungi, Thiazines, Rats, Inbred Strains, Microbial Sensitivity Tests, Triazoles, Rats, Chemistry, Mice, Thiazoles, Superoxides, Animals
Abstract

Starting from 3-aryl-4-amino-5-mercapto-4H-1,2,4-triazoles (II), two series of 3,6-disubstituted 7H-1,2,4-triazol [3,4-b] [1,3,4] thiadiazines (III) and their 5-carboxymethylthio derivatives (IV) were prepared. From the mercapto-amino-triazoles (II) because of their reactivity in some oxidising media, were obtained the triazole derivatives (V), (VI) and (VII). The synthesis of the alpha-thioketones (VIII) of 3-aryl-5-mercapto-1,3,4-oxadiazoles (I), used in alternative synthesis of triazole-thiadiazines (III), is also reported. All the substances described were subjected to biological screening. In the tests, the carboxymethylthiotriazole (IV) showed weak antiinflammatory activity (carrageenin edema) and more consistent scavanger activity, in vitro, on superoxide anions. The triazole-thiadiazines (III) and triazoles (II), (V) and (VI) showed moderate antimycotic activity.

Published
1987

41. ChemInform Abstract: Synthesis and Pharmacological Study of a Series of 3(2H)-Pyridazinones as Analgesic and Antiinflammatory Agents

Author

A. Caruso, Amico-Roxas M, S. Trombadore, Duro F, and Santagati Na

Subjects
Chemistry, Analgesic, Phenylbutazone, medicine, General Medicine, Antipyretic, Pharmacology, medicine.drug
Abstract

The synthesis and the pharmacological evaluation of some 3(2H)-pyridazinone derivatives are reported. The compounds were screened for analgesic, antiinflammatory and antipyretic activities. All tested derivatives showed a higher analgesic activity than phenylbutazone, while being devoid of ulcerogenic action.

Published
1986
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46. Influence of hyperprolactinemia induced by adenopituitary transplantation under the kidney capsule on the glutamic acid decarboxylase activity in various brain regions

Author

Nicoletti, F., Di Giorgio, R. M., Patti, F., Rampello, L., Daniele Filippo Condorelli, Amico-Roxas, M., Canonico, P. L., and Scapagnini, U.

Subjects
Animals, Brain, enzymology, Carboxy-Lyases, metabolism, Glutamate Decarboxylase, metabolism, Kidney, physiology, Male, Pituitary Gland, Anterior, physiology/transplantation, Prolactin, blood, Rats, Transplantation, Homologous, kidney, prolactin, brain, enzymology, pituitary gland, anterior, animals, blood, carboxy-lyases, glutamate decarboxylase, homologous, male, metabolism, physiology, physiology/transplantation, rats, transplantation, Pituitary Gland, Anterior, Transplantation, Homologous
Abstract

Glutamic acid decarboxylase activity was assayed in rat substantia nigra, corpus striatum, medial basal hypothalamus and cerebellum under conditions of hyperprolactinemia induced by transplantation of adenopituitary under the kidney capsule. The results indicate that hyperprolactinemia induces a slight increase in the glutamic acid decarboxylase activity of substantia nigra and medial basal hypothalamus and a more evident increase at striatal level. No change was observed in the cerebellum.

Published
1981

47. ChemInform Abstract: Synthesis and Pharmacological Activity of 2-Arylethenylthiazol-4-acetic Acids and -4-carboxylic Acids

Author

A. Caruso, Francesco Guerrera, S. Trombadore, Bonina F, Pappalardo F, Maria Angela Siracusa, and Amico-Roxas M

Subjects
chemistry.chemical_compound, chemistry, Stereochemistry, medicine, Alkoxy group, General Medicine, Antipyretic, Benzene, Ring (chemistry), Medicinal chemistry, medicine.drug
Abstract

Two new series of 2-aryletenylthiazolo-4-acetic (IV-XII) and 4-carboxylic (XIII-XXI) acids substituted with alkoxy groups in the benzene ring were synthesized. The compounds were subjected to comparative tests of antiinflammatory, analgesic and antipyretic activity.

Published
1986
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